Novel Cyclopropapyrroloindole Derivative (AT-3510) Bearing Methoxycarbonyl and Trifluoromethyl Groups
Copyright policy )Novel Cyclopropapyrroloindole Derivative (AT-3510) Bearing Methoxycarbonyl and Trifluoromethyl Groups
The seco-Cl 3-methoxycarbonyl-2-trifluoromethylcyclopropapyrroloindole (MCTFCPI) derivatives dl- and/or (S)-10 carrying various acyl moieties at the N6-position were synthesized along with their prodrugs (S)-12, and their antitumor activity was evaluated. Among these derivatives, AT-3510 [(S)-12m], the novel prodrug MCTFCPI derivative carrying a 5-(7-methoxybenzofuran-2-ylcarbonyl)aminoindole-2-carb onyl group at the N6-position, was found to exhibit more excellent antitumor activity against human tumor xenografts than the clinical trial candidates carzelesin (6) and KW-2189 (7) and cisplatin.
- Central Research Laboratories (United Kingdom) United Kingdom
Mice, Inbred BALB C, Transplantation, Heterologous, Antineoplastic Agents, Stereoisomerism, Mice, Structure-Activity Relationship, Tumor Cells, Cultured, Animals, Humans, Female, Prodrugs, Pyrroles, Drug Screening Assays, Antitumor, Benzofurans
Mice, Inbred BALB C, Transplantation, Heterologous, Antineoplastic Agents, Stereoisomerism, Mice, Structure-Activity Relationship, Tumor Cells, Cultured, Animals, Humans, Female, Prodrugs, Pyrroles, Drug Screening Assays, Antitumor, Benzofurans
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